Modified release formulations of antihypertensive drugs

a technology of antihypertensive drugs and modified release formulations, applied in the field of propranolol compound, can solve the problems of difficult control of the release of the difficulty of putting into the modified release formulation, and the difficulty of achieving the effect of reducing the risk of cardiovascular diseas

Inactive Publication Date: 2007-04-12
CAPRICORN PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0020] In one aspect, the one or more pharmaceutically acceptable exicipients may be selected from the group consisting of: microcrystalline cellulose, dibasic calcium phosphate dihydrate, starch, sodium starch glycolate, crospovidone, croscarmellose sodium, magnesium stearate, lactose, maleic acid, colloidal silicon dioxide, talc, and glyceryl behenate, or a mixture thereof.

Problems solved by technology

While propanolol has been used for many years as an active agent in an immediate release dosage form to control hypertension, it has proven very difficult to put into a modified release formulation.
No generic drug company has ever successfully created a modified release propanolol formulation that has been approved by the FDA as bioequivalent to INDERAL LA®.
This could be due to the relative high water solubility of the propranolol hydrochloride molecule which makes it difficult to control its release.
Perhaps another factor is the complexity of these prior art disclosures in terms of their formulation and manufacturing steps.

Method used

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  • Modified release formulations of antihypertensive drugs
  • Modified release formulations of antihypertensive drugs
  • Modified release formulations of antihypertensive drugs

Examples

Experimental program
Comparison scheme
Effect test

example 1

Granulation

[0084] Propranolol HCl (160 mg) and Microcrystalline cellulose powder (101.82 mg) are mixed into a blend with a high shear granulator for 15 minutes. A clear binder solution of ethyl cellulose N100 (8.44 mg) in sufficient amount of Isopropyl alcohol is made. The blend is further granulated with slow addition of the binder solution for 45 min. The granules are dried in a Thelco lab dryer at about 50° C. for about 1 hour. A sufficient amount of water is then added to facilitate extrusion. The resulting mass is extruded through a 1 mm mesh and then spheronized in a spheronizer to create granules. The granules are again dried in a Thelco lab dryer at about 50° C. till the moisture content is less than about 1.0% and solvent content is less than about 0.1% to yield beads with average of 850 um. The beads are then film-coated with a solution of ethylcellulose N100 (14.55 mg) in isopropyl alcohol with triethyl citrate (1.46 mg) as plasticizer in a conventional coating pan. The ...

example 2

Fluid Bed Coating

[0086] Propanolol containing cores are prepared as in Example No. 1. The cores containing 160 mg of propranolol hydrochloride are then coated with a solution of Methocel E5 LV premium (3.24 mg) and Ethylcellulose N100 (7.57 mg) in methanol with triethyl citrate (1.08 mg) as plasticizer coating layer using a fluid bed apparatus. A Glatt GPCG 3.1 can be used for this purpose. Fill the capsule size “1” with sufficient amount of beads so that the total Propranolol HCl content is 160 mg.

[0087] Dissolution was conducted according to the protocol set forth in Example 10. The results thereof are shown in graphical form in FIG. 2.

example 3

[0088] Propranolol hydrochloride 120 mg is used per dosage form which may be prepared similar to Example 1, except for the difference in dosage amount and the corresponding differences in the inactive ingredients. Alternatively, the quantity of the beads of Example 1 or 2 may be adjusted proportionately to provide 120 mg of the dose of propranolol hydrochloride.

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Abstract

Modified or extended release formulations containing propanolol compounds and associated methods are disclosed and described. In some aspects, such formulations may be substantially bioequivalent to known FDA approved propanolol formulations such as INDERAL LA®.

Description

PRIORITY DATA [0001] This application claims the benefit of U.S. Provisional Patent Application Ser. No. 60 / 685,788, filed on May 31, 2005, which is incorporated herein by reference.FIELD OF THE INVENTION [0002] The present invention relates to propranolol compound containing formulations with desired in-vitro and in-vivo characteristics which are simple to formulate and economical to manufacture on a commercial scale. Accordingly, the present invention involves the field of pharmaceutical sciences. BACKGROUND OF THE INVENTION [0003] Modified release propranolol formulations are desirable because they can achieve better control of hypertension for a longer period of time compared to immediate release formulations which often require multiple dosings in a single day. Examples of various known modified release propranolol formulations may be found in U.S. Pat. Nos. 6,337,091; 5,968,554; and 5,508,043, each of which are incorporated by reference. [0004] While propanolol has been used f...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/22
CPCA61K9/4808A61K9/5047A61K9/5089A61K31/138
Inventor CHERUKURI, S. RAORAVELLI, VITTORINO
Owner CAPRICORN PHARMA INC
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